WO2011028864A1 - Jak2 inhibitors and their use for the treatment of myeloproliferative diseases and cancer - Google Patents

Jak2 inhibitors and their use for the treatment of myeloproliferative diseases and cancer Download PDF

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Publication number
WO2011028864A1
WO2011028864A1 PCT/US2010/047621 US2010047621W WO2011028864A1 WO 2011028864 A1 WO2011028864 A1 WO 2011028864A1 US 2010047621 W US2010047621 W US 2010047621W WO 2011028864 A1 WO2011028864 A1 WO 2011028864A1
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WO
WIPO (PCT)
Prior art keywords
alkyl
methyl
ethyl
dihydroimidazo
carboxamide
Prior art date
Application number
PCT/US2010/047621
Other languages
English (en)
French (fr)
Inventor
Ashok V. Purandare
James W. Grebinski
Amy Hart
Jennifer Inghrim
Gretchen Schroeder
Honghe Wan
Original Assignee
Bristol-Myers Squibb Company
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to DK10757878.3T priority Critical patent/DK2473510T3/da
Priority to SI201030748T priority patent/SI2473510T1/sl
Priority to EA201270373A priority patent/EA022488B1/ru
Priority to JP2012528031A priority patent/JP5567137B2/ja
Priority to SG2012013900A priority patent/SG178591A1/en
Priority to EP10757878.3A priority patent/EP2473510B1/en
Priority to KR1020127008468A priority patent/KR101669311B1/ko
Priority to CA2772616A priority patent/CA2772616C/en
Priority to CN201080049628.0A priority patent/CN102596954B/zh
Priority to AU2010289497A priority patent/AU2010289497B2/en
Application filed by Bristol-Myers Squibb Company filed Critical Bristol-Myers Squibb Company
Priority to PL10757878T priority patent/PL2473510T3/pl
Priority to MX2012002480A priority patent/MX2012002480A/es
Priority to ES10757878.3T priority patent/ES2505270T3/es
Priority to BR112012004970-4A priority patent/BR112012004970B1/pt
Priority to NZ598521A priority patent/NZ598521A/xx
Publication of WO2011028864A1 publication Critical patent/WO2011028864A1/en
Priority to TNP2012000062A priority patent/TN2012000062A1/en
Priority to IL218115A priority patent/IL218115A/en
Priority to ZA2012/02384A priority patent/ZA201202384B/en
Priority to HRP20140814AT priority patent/HRP20140814T1/hr
Priority to SM201400148T priority patent/SMT201400148B/xx

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
PCT/US2010/047621 2009-09-03 2010-09-02 Jak2 inhibitors and their use for the treatment of myeloproliferative diseases and cancer WO2011028864A1 (en)

Priority Applications (20)

Application Number Priority Date Filing Date Title
PL10757878T PL2473510T3 (pl) 2009-09-03 2010-09-02 Inhibitory JAK2 i ich zastosowanie do leczenia chorób mieloproliferacyjnych i nowotworu
SI201030748T SI2473510T1 (sl) 2009-09-03 2010-09-02 Jak2 inhibitorji in njihova uporaba za zdravljenje mieloproliferativnih bolezni in raka
JP2012528031A JP5567137B2 (ja) 2009-09-03 2010-09-02 Ｊａｋ２阻害剤、ならびに骨髄増殖性疾患および癌の治療のためのそれらの使用
SG2012013900A SG178591A1 (en) 2009-09-03 2010-09-02 Jak2 inhibitors and their use for the treatment of myeloproliferative diseases and cancer
EP10757878.3A EP2473510B1 (en) 2009-09-03 2010-09-02 Jak2 inhibitors and their use for the treatment of myeloproliferative diseases and cancer
KR1020127008468A KR101669311B1 (ko) 2009-09-03 2010-09-02 Ｊａｋ２ 억제제, 및 골수증식성 질환 및 암의 치료를 위한 그의 용도
CA2772616A CA2772616C (en) 2009-09-03 2010-09-02 Jak2 inhibitors and their use for the treatment of myeloproliferative diseases and cancer
MX2012002480A MX2012002480A (es) 2009-09-03 2010-09-02 Inhibidores de jak2 y su uso en el tratamiento de enfermedades mieloproliferativas y cancer.
AU2010289497A AU2010289497B2 (en) 2009-09-03 2010-09-02 JAK2 inhibitors and their use for the treatment of myeloproliferative diseases and cancer
DK10757878.3T DK2473510T3 (da) 2009-09-03 2010-09-02 Jak-2-hæmmere og anvendelse heraf til behandling af myeloproliferativesygdomme og cancer
EA201270373A EA022488B1 (ru) 2009-09-03 2010-09-02 Ингибиторы jak2 и их применение для лечения миелопролиферативных заболеваний и злокачественной опухоли
CN201080049628.0A CN102596954B (zh) 2009-09-03 2010-09-02 Jak2抑制剂及其用于治疗骨髓增生性疾病及癌症的用途
ES10757878.3T ES2505270T3 (es) 2009-09-03 2010-09-02 Inhibidores de JAK2 y su uso para el tratamiento de enfermedades mieloproliferativas y cáncer
BR112012004970-4A BR112012004970B1 (pt) 2009-09-03 2010-09-02 Inibidores de jak2, seu uso no tratamento de doenças mieloproliferativas e câncer composição farmacêutica que os compreende
NZ598521A NZ598521A (en) 2009-09-03 2010-09-02 Jak2 inhibitors and their use for the treatment of myeloproliferative diseases and cancer
TNP2012000062A TN2012000062A1 (en) 2009-09-03 2012-02-10 Jak 2 inhibitors and their use for the treatment of myeloproliferative deseases and cancer
IL218115A IL218115A (en) 2009-09-03 2012-02-14 2jak inhibitors and their use in the preparation of medicines for the treatment of myelin growth and cancer
ZA2012/02384A ZA201202384B (en) 2009-09-03 2012-04-02 Jak2 inhibitors and their use for the treatment of myeloproliferative diseases and cancer
HRP20140814AT HRP20140814T1 (hr) 2009-09-03 2014-08-28 Inhibitori jak2 i njihova uporaba za lijeäśenje mijeloproliferativnih bolesti i karcinoma
SM201400148T SMT201400148B (it) 2009-09-03 2014-10-16 Inibitori di jak2 e loro uso per il trattamento del cancro e di malattie mieloproliferative

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US23950109P 2009-09-03 2009-09-03
US61/239,501 2009-09-03

Publications (1)

Publication Number Publication Date
WO2011028864A1 true WO2011028864A1 (en) 2011-03-10

Family

ID=42989674

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2010/047621 WO2011028864A1 (en) 2009-09-03 2010-09-02 Jak2 inhibitors and their use for the treatment of myeloproliferative diseases and cancer

Country Status (28)

Country Link
US (2) US8202881B2 (pt)
EP (1) EP2473510B1 (pt)
JP (2) JP5567137B2 (pt)
KR (1) KR101669311B1 (pt)
CN (1) CN102596954B (pt)
AR (1) AR078157A1 (pt)
AU (1) AU2010289497B2 (pt)
BR (1) BR112012004970B1 (pt)
CA (1) CA2772616C (pt)
CL (1) CL2012000589A1 (pt)
CO (1) CO6612228A2 (pt)
DK (1) DK2473510T3 (pt)
EA (1) EA022488B1 (pt)
ES (1) ES2505270T3 (pt)
HR (1) HRP20140814T1 (pt)
IL (1) IL218115A (pt)
MX (1) MX2012002480A (pt)
NZ (1) NZ598521A (pt)
PE (1) PE20121150A1 (pt)
PL (1) PL2473510T3 (pt)
PT (1) PT2473510E (pt)
SG (1) SG178591A1 (pt)
SI (1) SI2473510T1 (pt)
SM (1) SMT201400148B (pt)
TN (1) TN2012000062A1 (pt)
TW (2) TWI434848B (pt)
WO (1) WO2011028864A1 (pt)
ZA (1) ZA201202384B (pt)

Cited By (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014118388A1 (en) 2013-02-04 2014-08-07 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for assaying jak2 activity in red blood cells and uses thereof
WO2014193865A1 (en) * 2013-05-30 2014-12-04 Bristol-Myers Squibb Company Crystalline form of n,n-dicyclopropyl-4-(1,5-dimethyl-1 h-pyrazol-3-ylamino)-6-ethyl-1 -methyl-1,6-dihydroimidazo[4,5- d]fy rrolo[2,3-b]pyridine-7-carboxamide for the treatment of myeloproliferative disorders
WO2014193881A1 (en) * 2013-05-30 2014-12-04 Bristol-Myers Squibb Company Crystalline form of n,n-dicyclopropyl-4-(1,5-dimethyl-1 h-pyrazol-3-ylamino)-6-ethyl-1 -methyl-1,6-dihyrdroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide for the treatment of myeloproliferative disorders
WO2014193887A1 (en) * 2013-05-30 2014-12-04 Bristol-Myers Squibb Company Crystalline form of n,n-dicyclopropyl-4-(1,5-dimethyl-1 h-pyrazol-3-ylamino)-6-ethyl-1 -methyl-1,6-dihydroimidazo[4,5 d]fy rrolo[2,3-b]pyridine-7-carboxamide for the treatment of myeloproliferative disorders
WO2014193866A1 (en) * 2013-05-30 2014-12-04 Bristol-Myers Squibb Company Crystalline form of n,n-dicyclopropyl-4-(1,5-dimethyl-1 h-pyrazol-3-ylamino)-6-ethyl-1 -methyl-1,6-dihydroimidazo[4,5- d]fy rrolo[2,3-b]pyridine-7-carboxamide for the treatment of myeloproliferative disorders
WO2017013270A1 (en) 2015-07-23 2017-01-26 Universite De Strasbourg Use of leptin signaling inhibitor for protecting kidneys from patients having ciliopathy
WO2018167283A1 (en) 2017-03-17 2018-09-20 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma associated neural remodeling
WO2018189335A1 (en) 2017-04-13 2018-10-18 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
WO2022006457A1 (en) * 2020-07-02 2022-01-06 Incyte Corporation Tricyclic urea compounds as jak2 v617f inhibitors
US11661422B2 (en) 2020-08-27 2023-05-30 Incyte Corporation Tricyclic urea compounds as JAK2 V617F inhibitors
US11691971B2 (en) 2020-06-19 2023-07-04 Incyte Corporation Naphthyridinone compounds as JAK2 V617F inhibitors
US11753413B2 (en) 2020-06-19 2023-09-12 Incyte Corporation Substituted pyrrolo[2,1-f][1,2,4]triazine compounds as JAK2 V617F inhibitors
US11767323B2 (en) 2020-07-02 2023-09-26 Incyte Corporation Tricyclic pyridone compounds as JAK2 V617F inhibitors
US11919908B2 (en) 2020-12-21 2024-03-05 Incyte Corporation Substituted pyrrolo[2,3-d]pyrimidine compounds as JAK2 V617F inhibitors
US11958861B2 (en) 2021-02-25 2024-04-16 Incyte Corporation Spirocyclic lactams as JAK2 V617F inhibitors

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA022488B1 (ru) * 2009-09-03 2016-01-29 Бристол-Майерс Сквибб Кампани Ингибиторы jak2 и их применение для лечения миелопролиферативных заболеваний и злокачественной опухоли
WO2014093623A1 (en) * 2012-12-12 2014-06-19 University Of Washington Through Its Center For Commercialization Method and assays for cancer prognosis using jak2
WO2015031562A1 (en) 2013-08-29 2015-03-05 Bristol-Myers Squibb Company PROCESS FOR THE PREPARATION OF N,N-DICYCLOPROPYL-4-(1,5-DIMETHYL-1H-PYRAZOL-3-YLAMINO)-6-ETHYL-1-METHYL-1,6-DIHYDROIMIDAZO[4,5-d]PYRROLO[2,3-b]PYRIDINE-7-CARBOXAMIDE
WO2016024232A1 (en) 2014-08-11 2016-02-18 Acerta Pharma B.V. Therapeutic combinations of a btk inhibitor, a pi3k inhibitor, a jak-2 inhibitor and/or a cdk 4/6 inhibitor
PL3179991T3 (pl) 2014-08-11 2022-02-14 Acerta Pharma B.V. Kombinacje terapeutyczne inhibitora btk i inhibitora bcl-2
WO2016024231A1 (en) 2014-08-11 2016-02-18 Acerta Pharma B.V. Therapeutic combinations of a btk inhibitor, a pi3k inhibitor, a jak-2 inhibitor, a pd-1 inhibitor and/or a pd-l1 inhibitor
JOP20190144A1 (ar) 2016-12-16 2019-06-16 Janssen Pharmaceutica Nv إيميدازو بيرولو بيريدين كمثبطات لعائلة jak الخاصة بإنزيمات الكيناز
TW202016110A (zh) 2018-06-15 2020-05-01 比利時商健生藥品公司 Ｊａｋ激酶家族之小分子抑制劑
CN110483514B (zh) * 2019-09-16 2022-06-14 启元生物(杭州)有限公司 一种氰基取代的环肼衍生物及其应用
CN115916207A (zh) * 2020-08-20 2023-04-04 轶诺(浙江)药业有限公司 一类五元并六元杂环化合物及其作为蛋白受体激酶抑制剂的用途
JP2023544678A (ja) * 2020-10-08 2023-10-25 ユニケム ラボラトリーズ リミテッド 置換三環系化合物
CN113880745A (zh) * 2021-11-03 2022-01-04 山东亿嘉农化有限公司 一种曲洛比利的制备方法
WO2023225586A2 (en) * 2022-05-19 2023-11-23 4M Therapeutics Inc. Novel azaphenantrhene derivatives as inhibitors of glycogen synthase kinase 3 for therapeutic use

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006122137A1 (en) 2005-05-10 2006-11-16 Bristol-Myers Squibb Company 1, 6 -dihydro- 1,3, 5, 6-tetraaza-as-indacene based tricyclic compounds and pharmaceutical compositions comprising same as inhibitors of ikk enzyme activity
WO2008079965A1 (en) * 2006-12-22 2008-07-03 Incyte Corporation Substituted heterocycles as janus kinase inhibitors

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5532261A (en) 1994-12-12 1996-07-02 Merck & Co., Inc. Carbapenem antibiotics, compositions containing such compounds and methods of use
TR200101395T2 (tr) * 1998-09-18 2001-11-21 Basf Ag. Kinaz engelleyiciler olarak 4-Aminopyrrolopyrimidin'ler
TWI271406B (en) * 1999-12-13 2007-01-21 Eisai Co Ltd Tricyclic condensed heterocyclic compounds, preparation method of the same and pharmaceuticals comprising the same
CN1897950A (zh) * 2003-10-14 2007-01-17 惠氏公司 稠合芳基和杂芳基衍生物及其使用方法
EP1910358A2 (en) * 2005-07-14 2008-04-16 Astellas Pharma Inc. Heterocyclic janus kinase 3 inhibitors
GB0526246D0 (en) * 2005-12-22 2006-02-01 Novartis Ag Organic compounds
EP2155742A1 (en) * 2007-04-18 2010-02-24 AstraZeneca AB 5-aminopyrazol-3-yl-3h-imidazo [4,5-b]pyridine derivatives and their use for the treatment of cancer
WO2009035575A1 (en) * 2007-09-11 2009-03-19 Merck & Co., Inc. Inhibitors of janus kinases
AU2008335761B2 (en) * 2007-12-13 2014-04-24 Merck Sharp & Dohme Corp. Inhibitors of janus kinases
AU2009219154A1 (en) * 2008-02-29 2009-09-03 Cylene Pharmaceuticals, Inc. Protein kinase modulators
EP2370407B1 (en) 2008-12-19 2014-06-18 Bristol-Myers Squibb Company Carbazole and carboline kinase inhibitors
EA022488B1 (ru) * 2009-09-03 2016-01-29 Бристол-Майерс Сквибб Кампани Ингибиторы jak2 и их применение для лечения миелопролиферативных заболеваний и злокачественной опухоли

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006122137A1 (en) 2005-05-10 2006-11-16 Bristol-Myers Squibb Company 1, 6 -dihydro- 1,3, 5, 6-tetraaza-as-indacene based tricyclic compounds and pharmaceutical compositions comprising same as inhibitors of ikk enzyme activity
WO2008079965A1 (en) * 2006-12-22 2008-07-03 Incyte Corporation Substituted heterocycles as janus kinase inhibitors

Non-Patent Citations (10)

* Cited by examiner, † Cited by third party
Title
"Remington's Pharmaceutical Sciences,17th ed.,", 1985, MACK PUBLISHING COMPANY
ABU T. KHAN ET AL., TETRAHEDRON LETTERS, vol. 47, 2006, pages 2751 - 2754
H. BUNDGAARD, ADVANCED DRUG DELIVERY REVIEWS, vol. 8, 1992, pages 1 - 38
H. BUNDGAARD: "A Textbook of Drug Design and Development", 1991, article "Design and Application of Prodrugs", pages: 113 - 191
H. BUNDGAARD: "Design ofProdrugs", 1985, ELSEVIER
K. WIDDER, ET AL.: "Methods in Enzymology", vol. 112, 1985, ACADEMIC PRESS, pages: 309 - 396
NICOLAS BROSSE ET AL., EUR. J. ORG. CHEM., 2003, pages 4757 - 4764
SO OK PARK ET AL., J. COMB. CHEM., vol. 11, 2009, pages 315 - 326
SYNLETT, 2008, pages 2331
TETRAHEDRON, 2003, pages 2631

Cited By (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014118388A1 (en) 2013-02-04 2014-08-07 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for assaying jak2 activity in red blood cells and uses thereof
WO2014193865A1 (en) * 2013-05-30 2014-12-04 Bristol-Myers Squibb Company Crystalline form of n,n-dicyclopropyl-4-(1,5-dimethyl-1 h-pyrazol-3-ylamino)-6-ethyl-1 -methyl-1,6-dihydroimidazo[4,5- d]fy rrolo[2,3-b]pyridine-7-carboxamide for the treatment of myeloproliferative disorders
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